Synonyms: compound 5g [PMID 23275831] [1] | RKI1447
Compound class:
Synthetic organic
Comment: RKI-1447 is a pyridylthiazole-based urea analogue designed in the search for novel and biologically active Rho-associated protein kinase inhibitors [1].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
|
Bioactivity Comments |
Compound 5g has potent off-target effects (IC50 < 10nM) on many protein kinases, including AKT1, Aurora kinase A, IKBKe, JAK2, GSK3β, LIMK1, MYLK, CDC42BPA, RPS6KB1, PAK1, PKA, PRK1, RSK1, SGK1 and TBK1 [1]. We map ROCK1 and ROCK2 as primary molecular targets as these were the intended focus of the medicinal chemistry study [1]. |
Selectivity at enzymes | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|